Gema Santamaría Núñez

Abstract 1773: PM54, a novel transcription inhibitor with promising broad-spectrum antitumor activity

Gema Santamaría Núñez, Tommy Darrière, Federico M. Ruiz, Carlos Fernández‐Tornero et autres

PM54, a novel synthetic member of the ecteinascidin family, is derived from lurbinectedin, a marine-derived compound recognized for its potential in cancer therapy. This study aimed to characterize the in vitro antitumor activity of PM54, elucidate its mechanism of action through transcriptomic …

es (code pays fourni par la source)

Pan-inhibition of super-enhancer-driven oncogenic transcription by next-generation synthetic ecteinascidins yields potent anti-cancer activity

Max Cigrang, Julian Obid, Maguelone Nogaret, Léane Seno et autres

The plasticity of cancer cells facilitates their ability to adopt heterogeneous differentiation states, posing a significant challenge to therapeutic interventions. Specific gene expression programs, driven in part by super-enhancers (SEs), underlie cancer cell states. Here we successfully inhibit SE-driven transcription in phenotypically …

fr, us, es, tw (code pays fourni par la source)

Unveiling the Mechanism of Lurbinectedin’s Action and Its Potential in Combination Therapies in Small Cell Lung Cancer

Antonio Calles, Emiliano Calvo, Gema Santamaría Núñez, Federico Costanzo et autres

Lurbinectedin is a selective inhibitor of oncogenic transcription approved for the treatment of adult patients with metastatic small cell lung cancer with disease progression on or after platinum-based chemotherapy. Preclinical data provide evidence for lurbinectedin exerting its actions in a unique manner …

es, ch, us, fr, tw (code pays fourni par la source)

From Sea Sponge to Clinical Trials: Starting the Journey of the Novel Compound PM742

Patricia G. Cruz, Rogelio Fernández, Raquel Rodríguez‐Acebes, Marta Martínez et autres

PM742 (1), a new chemical entity, has been isolated from the sponge Discodermia du Bocage collected in the Pacific Ocean. This compound showed strong in vitro cytotoxicity against several human tumor cell lines as well as a tubulin depolymerization mechanism of action, …

es (code pays fourni par la source)

Abstract 6243: The novel antitubulin agent PM534 exhibits potent antitumoral and antiangiogenic properties in vitro and in vivo

Marta Martínez, María José Muñoz-Alonso, Gema Santamaría Núñez, María José Guillén et autres

Abstract Background: Microtubule targeting agents have demonstrated to be very effective antitumoral drugs. The development of novel anti-tubulin agents with more efficient mechanisms of action presents several challenges due to their poor solubility, troublesome synthesis or purification, and toxicities. In this work, …

es (code pays fourni par la source)

Abstract 6239: PM534 is a novel microtubule-destabilizing agent with high affinity and potent antineoplastic properties

María A. Oliva, Beatriz Álvarez‐Bernad, Daniel Lucena‐Agell, Marta Martínez et autres

Abstract Background: Microtubule targeting compounds are a successful class of anticancer agents in the clinic. Although highly potent, the currently approved antitumor agents targeting tubulin present some drawbacks such as the development of acquired resistances, which remain an obstacle for an effective …

es (code pays fourni par la source)

Abstract 6247: Lurbinectedin shows potent activity in all four molecular subtypes of small cell lung cancer (SCLC) and POU2F3 and SLFN11 are biomarkers for a better response

Marta Martínez, Gema Santamaría Núñez, María José Guillén, D. R. Rueda et autres

Abstract Background - SCLC is the most aggressive lung cancer type and with the worst prognosis. There are four molecular subtypes based on the high expression of distinct transcription factors and with different therapeutic vulnerabilities. However, all share transcriptional addiction as pathogenic …

es (code pays fourni par la source)

Abstract 1622: Ecubectedin is a novel transcriptional inhibitor that displays potent antitumor effects in vitro and in vivo

Gema Santamaría Núñez, Marta Martínez, María José Guillén, Eva Maria Garrido-Martin et autres

Abstract Background - Ecubectedin (PM14) is a novel transcriptional inhibitor related to ecteinascidins family. In this work, we present its antiproliferative activity and mechanism of action. The in vitro antitumor activity obtained in cellular models has been also demonstrated in in vivo …

es (code pays fourni par la source)

Supplementary Table 1 from Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells

Gema Santamaría Núñez, Carlos Mario Genes Robles, Christophe Giraudon, Juan Fernando Martínez-Leal et autres

Growth inhibitory activity of lurbinectedin on different cancer cell lines.

Supplementary Figure 3 from Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells

Gema Santamaría Núñez, Carlos Mario Genes Robles, Christophe Giraudon, Juan Fernando Martínez-Leal et autres

Figure S3. NER machinery remains active in the presence of DRB. A dual incision assay (48) was performed by the co-incubation of NER (XPC, TFIIH, XPA, RPA, XPG and XPF) components with increasing amount of DRB (10, 20, 50 and 100µM).

Supplementary Figure legends from Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells

Gema Santamaría Núñez, Carlos Mario Genes Robles, Christophe Giraudon, Juan Fernando Martínez-Leal et autres

Supplementary Figure legends

Supplementary Figure 5 from Lurbinectedin Specifically Triggers the Degradation of Phosphorylated RNA Polymerase II and the Formation of DNA Breaks in Cancer Cells

Gema Santamaría Núñez, Carlos Mario Genes Robles, Christophe Giraudon, Juan Fernando Martínez-Leal et autres

Figure S5. (A) PM030779 did not induce RNA Pol II degradation and DNA breaks. For the kinetics of RNA synthesis A549 cells were treated with the compound or DMSO in normal growth medium for 0, 30, 45, 60, 90 and 120 minutes …